首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, DNA-binding and topoisomerase inhibitory activity of ruthenium(II) polypyridyl complexes.
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Synthesis, DNA-binding and topoisomerase inhibitory activity of ruthenium(II) polypyridyl complexes.

机译:钌(II)聚吡啶基配合物的合成,DNA结合和拓扑异构酶抑制活性。

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摘要

Two ruthenium(II) complexes [Ru(bpy)(2)(bfipH)](2+) (1) and [Ru(phen)(2)(bfipH)](2+) (2) have been synthesized and characterized. The DNA-binding behaviors of complexes were studied by using spectroscopic and viscosity measurements. Results suggested that the two complexes bind to DNA in an intercalative mode. Complexes 1 and 2 can efficiently photocleave pBR322 DNA in vitro under irradiation, singlet oxygen ((1)O(2)) was proved to contribute to the DNA photocleavage process. Topoisomerase inhibition and DNA strand passage assay confirmed that two Ru(II) complexes acted as efficient dual inhibitors of topoisomerases I and II. In MTT cytotoxicity studies, two Ru(II) complexes exhibited antitumor activity against BEL-7402, HeLa, MCF-7 tumor cells. The AO/EB staining assay indicated that Ru(II) complexes could induce the apoptosis of HeLa cells.
机译:已合成并表征了两种钌(II)配合物[Ru(bpy)(2)(bfipH)](2+)(1)和[Ru(phen)(2)(bfipH)](2+)(2) 。通过光谱和粘度测量研究了复合物的DNA结合行为。结果表明这两种复合物以插入模式与DNA结合。配合物1和2可以有效地体外照射下光解pBR322 DNA,单重态氧((1)O(2))被证明有助于DNA的光切割过程。拓扑异构酶抑制和DNA链传递测定证实,两种Ru(II)复合物可作为拓扑异构酶I和II的有效双重抑制剂。在MTT细胞毒性研究中,两种Ru(II)配合物对BEL-7402,HeLa,MCF-7肿瘤细胞表现出抗肿瘤活性。 AO / EB染色检测结果表明,Ru(II)复合物可诱导HeLa细胞凋亡。

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